Valsartan
Valsartan
Diovan; Entresto (in fixed-dose combination with sacubitril)
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Summary
Common uses
Hypertension0, Heart failure with reduced ejection fraction0, Post-myocardial infarction0
Pharmacy
Starting dose
80-160 mg PO once daily (40 mg BID in HFrEF, titrating up to 160 mg BID)
Preparations
40, 80, 160, 320 mg tablets; oral suspension
US FDA Max
320 mg/d (hypertension); 320 mg/d (HF)
Pharmacology
Routes
Oral
Onset
BP effect 2 hours; max at 4-6 weeks
Duration
24 hours
Half-life
~6 hours[1]
Bioavailability
~25% (oral; food reduces absorption ~40%)[1]
Pregnancy
Contraindicated in pregnancy (all trimesters); fetal renal injury, oligohydramnios, hypocalvaria, hypotension. Stop on detection[1]
Legal status
Rx-only in US
Purported mechanism
Valsartan is a selective AT1 angiotensin-II receptor antagonist; blocking AT1 produces vasodilation, decreased aldosterone, and reduced sodium retention without the bradykinin accumulation that drives ACE-inhibitor cough.0 Largely hepatically cleared (~80% biliary); no active metabolite. Sacubitril-valsartan (Entresto) combines an ARB with neprilysin inhibition for HFrEF and was a notable advance over the ARB-alone trial (PARADIGM-HF, 2014)[1].
References
- ↑ 1.0 1.1 1.2 1.3 FDA Prescribing Information, Diovan (valsartan), Novartis, current revision. https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021283s039lbl.pdf